Difference between old & new generation cephalosporin.
4 generation are available. 1 st against gram positive bacteria 2 nd & 3 rd more against gram negative ones 4 th against both. Ceftriaxone belongs to the 3 rd generation category.
MOA & Pharmacological properties Inhibition of cell wall synthesis in bacteria. Bacteriostatic Concentration- independent bactericidal activity. Clinically significant post antibiotic effect is not observed.
Pharmacokinetics Administration : I/M or I/V. Distribution: distributes very well into all body fluids. Adequate therapeutic levels in CSF are achieved. Half life: 7-8 hours. Excretion: bile. So, can be used in renal insufficiency. Crosses placental barrier.
Dose IM injection : 250mg/500mg/1gm IV injection: 250mg/500mg/1gm/2gm
Indications Lower respiratory tract infections : by S.pneumoniae, S. aureus, H.influenza, E.coli etc. UTIs: caused by E.coli, K.pneumoniae , etc. Uncomplicated gonorrhea: by N. gonorrhoeae , including both penicillinase & non penicillinase producing strains. Bone & joint infections.
Abdominal infections : caused by E.coli, K.pneumoniae. ( most strains of clostridium difficile are resistant) Agent of choice : in treatment of meningitis by meningo cocci , H.inluanzae , N.meningitidis . Surgical prophylaxis.
Adverse effects Generally well tolerated. Phlebitis. GI upset. Skin reactions…. Pruritis . Headache, dizziness. Pancreatitis Bilary precipitates. Colitis.
Contraindications B- lactam hypersensitivity. In neonates (<28days) : in hyperbilirubinemic neonates. Concomitant treatment with IV calcium.
Precautions Severe hepatic impairment. Pregnancy …. Category B. Over dosage Symptomatic treatment is given.
Compatibility & Stability Compatible with Flagyl (metronidazole hydrochloride). Not with vancomycin and amino glycosides. Sterile powder should be stored at room temperature and protected from light. The color of solution ranges from light yellow to amber, depending on the length of storage, concentration and diluents used.
Resistance If organisms lack a pepetidoglycan cell wall e.g. mycoplasma. Or organisms that produce ESBLs.